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National Institute of Environmental Health Sciences

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Publication Detail

Title: Facile synthesis of [11C]buprenorphine for positron emission tomographic studies of opioid receptors.

Authors: Lever, J R; Mazza, S M; Dannals, R F; Ravert, H T; Wilson, A A; Wagner Jr, H N

Published In Int J Rad Appl Instrum A, (1990)

Abstract: We have developed a simple and rapid method for the production of buprenorphine (BPN), a potent opioid partial agonist, labelled with carbon-11 at the 6-methoxy position. The procedure uses a precursor synthesized in high yield (89%) from BPN in two steps and employs [11C]iodomethane as the radiolabelling reagent. [11C]BPN of 97% radiochemical purity can be prepared in high specific activity (41 GBq/mumol; 1120 mCi/mumol) in a radiochemical yield of 10% at end-of-synthesis (not decay corrected). The [11C]BPN is available for use in studies of cerebral opioid receptors by positron emission tomography within 24 min from end-of-bombardment, including radiosynthesis, purification, formulation for i.v. injection and determination of specific activity.

PubMed ID: 2172186 Exiting the NIEHS site

MeSH Terms: Buprenorphine*; Carbon Radioisotopes*; Isotope Labeling/methods; Receptors, Opioid*; Tomography, Emission-Computed*

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